| Description | Cipralisant is a selective histamine H3 receptor antagonist in vivo, and an agonist in vitro (pKi: 9.9 for histamine H3 receptor; Ki: 0.47 nM for rat histamine H3 receptor). It has the potential for the treatment of attention-deficit hyperactivity disorder. |
| In vitro | Cipralisant acts as a full agonist at the recombinant rat histamine H3 receptor in vitro and potently inhibits forskolin-induced cAMP accumulation (EC50: 0.23 nM). Cipralisant increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50: 5.6 nM) [2]. |
| In vivo | Cipralisant (10 mg/kg, p.o.) blocks R-α-methylhistamine (a histamine H3 receptor agonist)-induced water intake in rats [2]. |
| Target activity | H3 receptor (rat):（ki）0.47 nM, H3 receptor:（pki）9.9 |
| Synonyms | GT-2331 |
| molecular weight | 216.32 |
| Molecular formula | C14H20N2 |
| CAS | 213027-19-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Tedford CE, et al. High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models. Eur J Pharmacol. 1998 Jun 26;351(3):307-11. 2. Ito S, et al. Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor. Eur J Pharmacol. 2006 Jan 4;529(1-3):40-6. |